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9.Alpha.-Fluorocortisol

9.Alpha.-Fluorocortisol - General Information

A synthetic mineralocorticoid with anti-inflammatory activity. [PubChem]

 

Pharmacology of 9.Alpha.-Fluorocortisol

9.Alpha.-Fluorocortisol is a synthetic adrenocortical steroid possessing very potent mineralocorticoid properties and high glucocorticoid activity. It is indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome. The physiologic action of fludrocortisone acetate is similar to that of hydrocortisone. However, the effects of fludrocortisone acetate, particularly on electrolyte balance, but also on carbohydrate metabolism, are considerably heightened and prolonged. Mineralocorticoids act on the distal tubules of the kidney to enhance the reabsorption of sodium ions from the tubular fluid into the plasma; they increase the urinary excretion of both potassium and hydrogen ions.

 

9.Alpha.-Fluorocortisol for patients

The physician should advise the patient to report any medical history of heart disease, high blood pressure, or kidney or liver disease and to report current use of any medicines to determine if these medicines might interact adversely with fludrocortisone acetate. Patients who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chicken pox or measles and, if exposed, to obtain medical advice. The patient's understanding of his steroid-dependent status and increased dosage requirement under widely variable conditions of stress is vital. Advise the patient to carry medical identification indicating his dependence on steroid medication and, if necessary, instruct him to carry an adequate supply of medication for use in emergencies. Stress to the patient the importance of regular follow-up visits to check his progress and the need to promptly notify the physician of dizziness, severe or continuing headaches, swelling of feet or lower legs, or unusual weight gain. Advise the patient to use the medicine only as directed, to take a missed dose as soon as possible, unless it is almost time for the next dose, and not to double the next dose.

9.Alpha.-Fluorocortisol Interactions

When administered concurrently, the following drugs may interact with adrenal corticosteroids.

Amphotericin B or potassium-depleting diuretics (benzothiadiazines and related drugs, ethacrynic acid and furosemide) enhanced hypokalemia. Check serum potassium levels at frequent intervals; use potassium supplements if necessary.

Digitalis glycosides enhanced possibility of arrhythmias or digitalis toxicity associated with hypokalemia. Monitor serum potassium levels; use potassium supplements if necessary.

Oral anticoagulants decreased prothrombin time response. Monitor prothrombin levels and adjust anticoagulant dosage accordingly.

Antidiabetic drugs (oral agents and insulin) diminished antidiabetic effect. Monitor for symptoms of hyperglycemia; adjust dosage of antidiabetic drug upward if necessary.

Aspirin increased ulcerogenic effect; decreased pharmacologic effect of aspirin. Rarely salicylate toxicity may occur in patients who discontinue steroids after concurrent high-dose aspirin therapy. Monitor salicylate levels or the therapeutic effect for which aspirin is given; adjust salicylate dosage accordingly if effect is altered.

Barbiturates, phenytoin, or rifampin increased metabolic clearance of fludrocortisone acetate because of the induction of hepatic enzymes. Observe the patient for possible diminished effect of steroid and increase the steroid dosage accordingly.

Anabolic steroids (particularly C-17 alkylated androgens such as oxymetholone, methandrostenolone, norethandrolone, and similar compounds) enhanced tendency toward edema. Use caution when giving these drugs together, especially in patients with hepatic or cardiac disease.

Vaccines neurological complications and lack of antibody response.

Estrogen increased levels of corticosteroid-binding globulin, thereby increasing the bound (inactive) fraction; this effect is at least balanced by decreased metabolism of corticosteroids. When estrogen therapy is initiated, a reduction in corticosteroid dosage may be required, and increased amounts may be required when estrogen is terminated.

 

Drug/Laboratory Test Interactions

Corticosteroids may affect the nitrobluetetrazolium test for bacterial infection and produce false-negative results.

 

9.Alpha.-Fluorocortisol Contraindications

Corticosteroids are contraindicated in patients with systemic fungal infections and in those with a history of possible or known hypersensitivity to these agents.

 

Additional information about 9.Alpha.-Fluorocortisol

9.Alpha.-Fluorocortisol Indication: For partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome.
Mechanism Of Action: 9.Alpha.-Fluorocortisol binds the mineralocorticoid receptor (aldosterone receptor). This binding (or activation of the mineralocorticoid receptor by fludrocortisone) in turn causes an increase in ion and water transport and thus raises extracellular fluid volume and blood pressure and lowers potassium levels.
Drug Interactions: Ambenonium The corticosteroid decreases the effect of anticholinesterases
Edrophonium The corticosteroid decreases the effect of anticholinesterases
Neostigmine The corticosteroid decreases the effect of anticholinesterases
Pyridostigmine The corticosteroid decreases the effect of anticholinesterases
Anisindione The corticosteroid alters the anticoagulant effect
Dicumarol The corticosteroid alters the anticoagulant effect
Acenocoumarol The corticosteroid alters the anticoagulant effect
Warfarin The corticosteroid alters the anticoagulant effect
Amobarbital The barbiturate decreases the effect of the corticosteroid
Aprobarbital The barbiturate decreases the effect of the corticosteroid
Butabarbital The barbiturate decreases the effect of the corticosteroid
Butalbital The barbiturate decreases the effect of the corticosteroid
Butethal The barbiturate decreases the effect of the corticosteroid
Dihydroquinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Heptabarbital The barbiturate decreases the effect of the corticosteroid
Hexobarbital The barbiturate decreases the effect of the corticosteroid
Methohexital The barbiturate decreases the effect of the corticosteroid
Methylphenobarbital The barbiturate decreases the effect of the corticosteroid
Pentobarbital The barbiturate decreases the effect of the corticosteroid
Phenobarbital The barbiturate decreases the effect of the corticosteroid
Primidone The barbiturate decreases the effect of the corticosteroid
Quinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Secobarbital The barbiturate decreases the effect of the corticosteroid
Talbutal The barbiturate decreases the effect of the corticosteroid
Trisalicylate-choline The corticosteroid decreases the effect of salicylates
Salicylate-magnesium The corticosteroid decreases the effect of salicylates
Salicylate-sodium The corticosteroid decreases the effect of salicylates
Salsalate The corticosteroid decreases the effect of salicylates
Aspirin The corticosteroid decreases the effect of salicylates
Bismuth Subsalicylate The corticosteroid decreases the effect of salicylates
Ethotoin The enzyme inducer decreases the effect of the corticosteroid
Fosphenytoin The enzyme inducer decreases the effect of the corticosteroid
Mephenytoin The enzyme inducer decreases the effect of the corticosteroid
Phenytoin The enzyme inducer decreases the effect of the corticosteroid
Rifampin The enzyme inducer decreases the effect of the corticosteroid
Midodrine Increased arterial pressure
Food Interactions: Avoid excess salt/sodium unless otherwise instructed by your physician.
Take with food to reduce irritation.
Generic Name: Fludrocortisone
Synonyms: Not Available
Drug Category: Anti-inflammatory Agents; Adrenergic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Fludrocortisone: 9 .Alpha. Ff; 9 Alpha Ff; 9 alpha-Fludrocortisone; 9 alpha-Fluorocortisol; 9.Alpha.-Fluorocortisol; 9.Alpha.-Fluorohydrocortisone; Alflorone; Astonin-H; F-COL; F-Cortef; Florinef; Fludrocortisona [Inn-Spanish]; Fludrocortisone Acetate; Fludrocortisonum [Inn-Latin]; Fludrocortone; Fludrone; Fludronef; Fluodrocortisone; Fluohydrisone; Fluohydrocortisone; Fluorocortisol; Fluorocortisone; ZK5;
Absorption: Not Available
Toxicity (Overdose): Effects of overexposure include irritation, cardiac edema, increased blood volume, hypertension, cardiac arrhythmias, enlargement of the heart, headaches, and weakness of the extremities.
Protein Binding: High
Biotransformation: Hepatic, some renal.
Half Life: 3.5 hours
Dosage Forms of 9.Alpha.-Fluorocortisol: Tablet Oral
Chemical IUPAC Name: (8S,9R,10S,11S,13S,14S,17R)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
Chemical Formula: C21H29FO5
Fludrocortisone on Wikipedia: http://en.wikipedia.org/wiki/Fludrocortisone
Organisms Affected: Humans and other mammals